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TitleStructural insights into the molecular effects of the anthelmintics monepantel and betaine on the Caenorhabditis elegans acetylcholine receptor ACR-23.
Journal, issue, pagesEMBO J, Vol. 43, Issue 17, Page 3787-3806, Year 2024
Publish dateJul 15, 2024
AuthorsFenglian Liu / Tianyu Li / Huihui Gong / Fei Tian / Yan Bai / Haowei Wang / Chonglin Yang / Yang Li / Fei Guo / Sheng Liu / Qingfeng Chen /
PubMed AbstractAnthelmintics are drugs used for controlling pathogenic helminths in animals and plants. The natural compound betaine and the recently developed synthetic compound monepantel are both anthelmintics ...Anthelmintics are drugs used for controlling pathogenic helminths in animals and plants. The natural compound betaine and the recently developed synthetic compound monepantel are both anthelmintics that target the acetylcholine receptor ACR-23 and its homologs in nematodes. Here, we present cryo-electron microscopy structures of ACR-23 in apo, betaine-bound, and betaine- and monepantel-bound states. We show that ACR-23 forms a homo-pentameric channel, similar to some other pentameric ligand-gated ion channels (pLGICs). While betaine molecules are bound to the classical neurotransmitter sites in the inter-subunit interfaces in the extracellular domain, monepantel molecules are bound to allosteric sites formed in the inter-subunit interfaces in the transmembrane domain of the receptor. Although the pore remains closed in betaine-bound state, monepantel binding results in an open channel by wedging into the cleft between the transmembrane domains of two neighboring subunits, which causes dilation of the ion conduction pore. By combining structural analyses with site-directed mutagenesis, electrophysiology and in vivo locomotion assays, we provide insights into the mechanism of action of the anthelmintics monepantel and betaine.
External linksEMBO J / PubMed:39009676 / PubMed Central
MethodsEM (single particle)
Resolution2.61 - 2.96 Å
Structure data

60063

8zfk

EMDB-60063, PDB-8zfk:
Caenorhabditis elegans ACR-23 in betaine and monepantel bound state
Method: EM (single particle) / Resolution: 2.64 Å

60064

8zfl

EMDB-60064, PDB-8zfl:
Caenorhabditis elegans ACR-23 in apo state
Method: EM (single particle) / Resolution: 2.61 Å

60065

8zfm

EMDB-60065, PDB-8zfm:
Caenorhabditis elegans ACR-23 in betaine bound state
Method: EM (single particle) / Resolution: 2.96 Å

Chemicals

ChemComp-NAG:
2-acetamido-2-deoxy-beta-D-glucopyranose

PDB-1d8e:
Zinc-depleted FTase complexed with K-RAS4B peptide substrate and FPP analog.

ChemComp-BET:
TRIMETHYL GLYCINE

ChemComp-HOH:
WATER

Source
  • caenorhabditis elegans (invertebrata)
  • escherichia coli (E. coli)
  • shimwellia blattae (bacteria)
KeywordsTRANSPORT PROTEIN / ion channel

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